scholarly journals Antinociceptive Activity of Methanolic Extract ofClinacanthus nutansLeaves: Possible Mechanisms of Action Involved

2018 ◽  
Vol 2018 ◽  
pp. 1-15 ◽  
Author(s):  
Zainul Amiruddin Zakaria ◽  
Mohammad Hafiz Abdul Rahim ◽  
Rushduddin Al Jufri Roosli ◽  
Mohd Hijaz Mohd Sani ◽  
Maizatul Hasyima Omar ◽  
...  
Keyword(s):  
Bioactive Compounds ◽  
Methanolic Extract ◽  
Cholinergic Receptors ◽  
Antinociceptive Activity ◽  
Receptor Subtypes ◽  
Dependent Manner ◽  
Opioid Receptor Subtypes ◽  
Glutamatergic Signaling ◽  
Clinacanthus Nutans ◽  
Dose Dependent

Methanolic extract ofClinacanthus nutansLindau leaves (MECN) has been proven to possess antinociceptive activity that works via the opioid and NO-dependent/cGMP-independent pathways. In the present study, we aimed to further determine the possible mechanisms of antinociception of MECN using various nociceptive assays. The antinociceptive activity of MECN was (i) tested against capsaicin-, glutamate-, phorbol 12-myristate 13-acetate-, bradykinin-induced nociception model; (ii) prechallenged against selective antagonist of opioid receptor subtypes (β-funaltrexamine, naltrindole, and nor-binaltorphimine); (iii) prechallenged against antagonist of nonopioid systems, namely,α2-noradrenergic (yohimbine),β-adrenergic (pindolol), adenosinergic (caffeine), dopaminergic (haloperidol), and cholinergic (atropine) receptors; (iv) prechallenged with inhibitors of various potassium channels (glibenclamide, apamin, charybdotoxin, and tetraethylammonium chloride). The results demonstrated that the orally administered MECN (100, 250, and 500 mg/kg) significantly (p<0.05) reversed the nociceptive effect of all models in a dose-dependent manner. Moreover, the antinociceptive activity of 500 mg/kg MECN was significantly (p<0.05) inhibited by (i) antagonists of μ-,δ-, andκ-opioid receptors; (ii) antagonists ofα2-noradrenergic, β-adrenergic, adenosinergic, dopaminergic, and cholinergic receptors; and (iii) blockers of different K+channels (voltage-activated-, Ca2+-activated, and ATP-sensitive-K+channels, resp.). In conclusion, MECN-induced antinociception involves modulation of protein kinase C-, bradykinin-, TRVP1 receptors-, and glutamatergic-signaling pathways; opioidergic,α2-noradrenergic,β-adrenergic, adenosinergic, dopaminergic, and cholinergic receptors; and nonopioidergic receptors as well as the opening of various K+channels. The antinociceptive activity could be associated with the presence of several flavonoid-based bioactive compounds and their synergistic action with nonvolatile bioactive compounds.

PHYTOCHEMICAL AND BIOLOGICAL STUDIES OF ROTULA AQUATICA LOUR. ROOTS

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (11) ◽  
pp. 34-38
Author(s):  
T. Shyam ◽  
◽  
S Ganapaty
Keyword(s):  
Body Weight ◽  
Spectroscopic Data ◽  
Methanolic Extract ◽  
Hepatoprotective Activity ◽  
Dependent Manner ◽  
Biological Studies ◽  
Bacteria And Fungi ◽  
Dose Levels ◽  
Dose Dependent ◽  
Chemical Evidence

Four compounds viz α-amyrin, β- amyrin, bauerenol and ellagic acid were isolated from the methanolic extract of Rotula aquatica roots. The structures of these compounds were elucidated on the basis of spectroscopic data analysis and chemical evidence. The extract was evaluated for hepatoprotective activity against carbon tetrachloride induced hepatotoxic model at a dose levels of 200,400 and 800 mg/ kg body weight and compared with that of the standard silymarin (25mg/kg body weight). It showed good hepatoprotective activity in a dose dependent manner. The extract was also screened for antimicrobial activity against various types of organisms like bacteria and fungi.

Antidiabetic and antioxidative properties of the hydro-methanolic extract (60:40) of rhizomes of Curcuma amada roxb. (Zingiberaceae) in streptozotocin-induced diabetic male albino rat: a dose-dependent study through biochemical and genomic approaches

2019 ◽  
Vol 16 (4) ◽  
Author(s):  
Dipanwita Mitra ◽  
Riya Sarkar ◽  
Debidas Ghosh
Keyword(s):  
Body Weight ◽  
Methanolic Extract ◽  
Fasting Blood Glucose ◽  
Diabetic Rats ◽  
Diabetic Group ◽  
Dependent Manner ◽  
Male Adult ◽  
Curcuma Amada ◽  
Corrective Effect ◽  
Dose Dependent

Abstract Background Curcuma amada is the most popular traditional medicine in India for the treatment of diabetes. The present study aimed to focus the antidiabetic and antioxidative activity of C. amada through the analysis of biochemical and genomic levels in a dose-dependent manner in streptozotocin-induced male adult rat. Method Streptozotocin-induced diabetic rats were administered orally with hydro-methanolic extract of C. amada at the dose of 10, 20, 40 and 80 mg/100 g body weight of rats for 28 days. The antidiabetic and antioxidative efficacy of the extract on glycemic, enzymatic, genomic and histological sensors along with toxicity study was investigated. Results The result showed a significant antidiabetic and antioxidative effect of the extract at dose-dependent manner. The significant recovery of fasting blood glucose level, serum insulin, activity of carbohydrate metabolic enzymes and antioxidative enzymes in extract-treated diabetic group as compared to untreated diabetic group were noted. After the extract treatment, the size of pancreatic islet and cell population densities were significantly increased. Activities of glutamate oxaloacetate transaminase and glutamate pyruvate transaminase in liver were significantly recovered along with the correction of Bax and Bcl-2 gene expression in hepatic tissue after the extract treatment in diabetic rats in respect to untreated diabetic group. Out of all the doses, the significant effects were noted at the dose of 20 mg/100 g body weight which has been considered as threshold dose in the concern. Conclusion It may be concluded that the significant and corrective effect in most of the sensors was noted at the minimum dose of 20 mg/100 g body weight of hydro-methanolic extract of C. amada without producing any toxicity.

scholarly journals Anthelmintic and Cytotoxic Activities of Two Medicinal Plants: Polygonum viscosum and Aphanamixis polystachya Growing in Bangladesh

2014 ◽  
Vol 6 (2) ◽  
pp. 339-345 ◽  
Author(s):  
M. N. Amin ◽  
M. S. Majumder ◽  
M. M. R. Moghal ◽  
S. Banik ◽  
A. Kar ◽  
...  
Keyword(s):  
Methanolic Extract ◽  
Anthelmintic Activity ◽  
Cytotoxic Activities ◽  
Dependent Manner ◽  
Reference Standard ◽  
Cytotoxic Potential ◽  
Lc50 Value ◽  
Vincristine Sulphate ◽  
Dose Dependent

The present study was designed to investigate in vitro anthelmintic and cytotoxic activities of crude methanolic extract of two plants(Polygonum viscosum and Aphanamixis polystachya) grown in Bangladesh. Evaluation of cytotoxic activity was done using the brine shrimp lethality bioassay. The crude methanolic extract of Polygonum viscosum showed significant cytotoxic potential (LC50 value of 6.34 ?g/ml) among all the fractions comparing with that of standard vincristine sulphate (0.825 ?g/ml). Besides, the LC50 values of crude methanolic extract, pet ether and chloroform extracts of Aphanamixis polystachya showed good cytotoxic activities 11, 10.36, and 16.45 µg/ml, respectively. The other study was undertaken to evaluate anthelmintic activity (using Pheretima posthuma model) where piperazine was used as reference standard. The crude methanolic extract of Polygonum viscosum leaves produced a significant anthelmintic activity in dose dependent manner and the activity of crude extract was comparable with that of standard drugs. Besides, the Aphanamixis polystachya extract revealed moderate anthelmintic activity. Here, the anova testing was done with the P < 0.05. Further studies are suggested to determine the active compounds responsible for the anthelmintic and cytotoxic activities of these two plant extracts.   Keywords: Anthelmintic; Cytotoxic; Medicinal plant; Aphanamixis polystachya; Polygonum viscosu.  © 2014 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved.   doi: http://dx.doi.org/10.3329/jsr.v6i2.17299 J. Sci. Res. 6 (2), 339-345 (2014) 

Characterization of adenosine receptor(s) involved in adenosine-induced bronchoconstriction in an allergic mouse model

2003 ◽  
Vol 284 (6) ◽  
pp. L1012-L1019 ◽  
Author(s):  
Ming Fan ◽  
Weixi Qin ◽  
S. Jamal Mustafa
Keyword(s):  
Mouse Model ◽  
Adenosine Receptor ◽  
Receptor Subtypes ◽  
Dependent Manner ◽  
Transcript Levels ◽  
Allergen Sensitization ◽  
Selective Agonist ◽  
Dose Dependent ◽  
Allergic Mouse

We recently reported that adenosine caused bronchoconstriction and enhanced airway inflammation in an allergic mouse model. In this study, we further report the characterization of the subtype of adenosine receptor(s) involved in bronchoconstriction. 5′-( N-ethylcarboxamido)adenosine (NECA), a nonselective adenosine agonist, elicited bronchoconstriction in a dose-dependent manner. Little effects of N 6-cyclopentyladenosine (A1-selective agonist) and 2- p-(2-carboxyethyl)phenethylamino-5′- N-ethylcarboxamidoadenosine (A2A-selective agonist) compared with NECA were observed in this model. 2-Chloro- N 6-(3-iodobenzyl)-9-[5-(methylcarbamoyl)-β-d-ribofuranosyl]adenosine, an A3-selective receptor agonist, produced a dose-dependent bronchoconstrictor response, which was blocked by selective A3 antagonist 2,3-diethyl-4,5-dipropyl-6-phenylpyridine-3-thiocarboxylate-5-carboxylate (MRS1523). However, MRS1523 only partially inhibited NECA-induced bronchoconstriction. Neither selective A1 nor A2A antagonists affected NECA-induced bronchoconstriction. Enprofylline, a relatively selective A2B receptor antagonist, blocked partly NECA-induced bronchoconstriction. Furthermore, a combination of enprofylline and MRS1523 completely abolished NECA-induced bronchoconstrictor response. Using RT-PCR, we found that all four adenosine receptor subtypes are expressed in control lungs. Allergen sensitization and challenge significantly increased transcript levels of the A2B and A3receptors, whereas the A1 receptor message decreased. No change in transcript levels of A2A receptors was observed after allergen sensitization and challenge. These findings suggest that A2B and A3 adenosine receptors play an important role in adenosine-induced bronchoconstriction in our allergic mouse model. Finally, whether the airway effects of the receptor agonists/antagonists are direct or indirect needs further investigations.

scholarly journals Antinociceptive Activity of Petroleum Ether Fraction of Clinacanthus nutans Leaves Methanolic Extract: Roles of Nonopioid Pain Modulatory Systems and Potassium Channels

2019 ◽  
Vol 2019 ◽  
pp. 1-12 ◽  
Author(s):  
Zainul Amiruddin Zakaria ◽  
Mohammad Hafiz Abdul Rahim ◽  
Rushduddin Al Jufri Roosli ◽  
Mohd Hijaz Mohd Sani ◽  
Najihah Hanisah Marmaya ◽  
...  
Keyword(s):  
Petroleum Ether ◽  
Methanolic Extract ◽  
Antinociceptive Activity ◽  
Channel Blockers ◽  
Tetraethylammonium Chloride ◽  
Petroleum Ether Fraction ◽  
Ether Fraction ◽  
Clinacanthus Nutans ◽  
Antinociceptive Mechanisms ◽  
Derivatives Of

Methanolic extract of Clinacanthus nutans Lindau leaves (MECN) has been reported to exert antinociceptive activity. The present study aimed to elucidate the possible antinociceptive mechanisms of a lipid-soluble fraction of MECN, which was obtained after sequential extraction in petroleum ether. The petroleum ether fraction of C. nutans (PECN), administered orally to mice, was (i) subjected to capsaicin-, glutamate-, phorbol 12-myristate 13-acetate-, bradykinin-induced nociception model; (ii) prechallenged (intraperitoneal (i.p.)) with 0.15 mg/kg yohimbine, 1 mg/kg pindolol, 3 mg/kg caffeine, 0.2 mg/kg haloperidol, or 10 mg/kg atropine, which were the respective antagonist of α2-adrenergic, β-adrenergic, adenosinergic, dopaminergic, or muscarinic receptors; and (iii) prechallenged (i.p.) with 10 mg/kg glibenclamide, 0.04 mg/kg apamin, 0.02 mg/kg charybdotoxin, or 4 mg/kg tetraethylammonium chloride, which were the respective inhibitor of ATP sensitive-, small conductance Ca2+-activated-, large conductance Ca2+-activated-, or nonselective voltage-activated-K+ channel. Results obtained demonstrated that PECN (100, 250, and 500 mg/kg) significantly (P<0.05) inhibited all models of nociception described earlier. The antinociceptive activity of 500 mg/kg PECN was significantly (P<0.05) attenuated when prechallenged with all antagonists or K+ channel blockers. However, only pretreatment with apamin and charybdotoxin caused full inhibition of PECN-induced antinociception. The rest of the K+ channel blockers and all antagonists caused only partial inhibition of PECN antinociception, respectively. Analyses on PECN’s phytoconstituents revealed the presence of antinociceptive-bearing bioactive compounds of volatile (i.e., derivatives of γ–tocopherol, α–tocopherol, and lupeol) and nonvolatile (i.e., cinnamic acid) nature. In conclusion, PECN exerts a non-opioid-mediated antinociceptive activity involving mainly activation of adenosinergic and cholinergic receptors or small- and large-conductance Ca2+-activated-K+ channels.

Mast Cell Stabilizing, Antianaphylactic and Bronchodilatory activity of Methanolic extract of Averrhoa carambola Fruit

2021 ◽  
pp. 5258-5263
Author(s):  
Ravindra Babu Sajja ◽  
Prasad Konduri ◽  
Eswar Kumar Kilari
Keyword(s):  
Mast Cell ◽  
Methanolic Extract ◽  
Mast Cell Degranulation ◽  
Dependent Manner ◽  
Averrhoa Carambola ◽  
Peritoneal Mast Cells ◽  
Antianaphylactic Activity ◽  
Phytochemical Studies ◽  
Dose Dependent ◽  
Mast Cell Stabilization

This work was mainly aimed to study the mast cell stabilizing, anti-anaphylactic and bronchodilatory activities of methanolic extract of Averrhoa carambola (ACME). Mast cell stabilization activity was investigated by Compound 48/80 induced mast cell degranulation in rats and antianaphylactic activity was performed by determining the mortality rate of mice upon exposure to compound 48/80. The bronchodilatory effect of ACME was studied on histamine aerosol-induced bronchospasm using guinea pigs, in which occurrence of preconvulsive dyspnea (PCD) was noted as end point. Treatment with ACME (100, 200 and 400mg/kg) showed significant (p<0.05) protection of rat peritoneal mast cells and significantly (p<0.05) reduced the mortality of mice in a dose dependent manner. ACME significantly (p<0.05) increased the time of preconvulsive dyspnea (PCD) in a dose dependent manner that suggestive of bronchodilating activity. Phytochemical studies observed presence of saponins, tannins, steroids, alkaloids, flavonoids and glycosides. From these finding, we concluded that ACME possesses mast cell stabilizing; anti anaphylactic and bronchodilatory activity which might be used in treatment of asthma.

Melanin-concentrating hormone: a functional melanocortin antagonist in the hypothalamus

1998 ◽  
Vol 274 (4) ◽  
pp. E627-E633 ◽  
Author(s):  
David S. Ludwig ◽  
Kathleen G. Mountjoy ◽  
Jeffrey B. Tatro ◽  
Jennifer A. Gillette ◽  
Robert C. Frederich ◽  
...  
Keyword(s):  
Food Intake ◽  
Mammalian Brain ◽  
Receptor Subtypes ◽  
Dependent Manner ◽  
Intracerebroventricular Administration ◽  
Melanocyte Stimulating Hormone ◽  
Molar Excess ◽  
Melanin Concentrating Hormone ◽  
Skin Coloration ◽  
Dose Dependent

Melanin-concentrating hormone (MCH) and α-melanocyte-stimulating hormone (α-MSH) demonstrate opposite actions on skin coloration in teleost fish. Both peptides are present in the mammalian brain, although their specific physiological roles remain largely unknown. In this study, we examined the interactions between MCH and α-MSH after intracerebroventricular administration in rats. MCH increased food intake in a dose-dependent manner and lowered plasma glucocorticoid levels through a mechanism involving ACTH. In contrast, α-MSH decreased food intake and increased glucocorticoid levels. MCH, at a twofold molar excess, antagonized both actions of α-MSH. α-MSH, at a threefold molar excess, blocked the orexigenic properties of MCH. MCH did not block α-MSH binding or the ability of α-MSH to induce cAMP in cells expressing either the MC3 or MC4 receptor, the principal brain α-MSH receptor subtypes. These data suggest that MCH and α-MSH exert opposing and antagonistic influences on feeding behavior and the stress response and may function in a coordinate manner to regulate metabolism through a novel mechanism mediated in part by an MCH receptor.

scholarly journals Methanolic Extract of Ceplukan Leaf (Physalis minimaL.) Attenuates Ventricular Fibrosis through Inhibition of TNF-αin Ovariectomized Rats

2016 ◽  
Vol 2016 ◽  
pp. 1-7 ◽  
Author(s):  
Bayu Lestari ◽  
Nur Permatasari ◽  
Mohammad Saifur Rohman
Keyword(s):  
Heart Failure ◽  
Treatment Group ◽  
Wistar Rats ◽  
Methanolic Extract ◽  
Ovariectomized Rats ◽  
Dependent Manner ◽  
Estrogen Level ◽  
Menopausal Women ◽  
Ventricular Fibrosis ◽  
Dose Dependent

The increase of heart failure prevalence on menopausal women was correlated with the decrease of estrogen level. The aim of this study is to investigate the effects of ceplukan leaf (Physalis minimaL.), which contains phytoestrogen physalin and withanolides, on ventricular TNF-αlevel and fibrosis in ovariectomized rats. Wistar rats were divided into six groups (control (—); OVX 5: 5-week ovariectomy (OVX); OVX 9: 9-week ovariectomy; treatments I, II, and III: 9-weeks OVX + 4-week ceplukan leaf’s methanolic extract doses 500, 1500, and 2500 mg/kgBW, resp.). TNF-αlevels were measured with ELISA. Fibrosis was counted as blue colored tissues percentage using Masson’s Trichrome staining. This study showed that prolonged hypoestrogen increases ventricular fibrosis (p<0.05). Ceplukan leaf treatment also resulted in a decrease of ventricular fibrosis and TNF-αlevel in dose dependent manner compared to without treatment group (p<0.05). Furthermore, the TNF-αlevel was normalized in 2500 mg/kgBWPhysalis minimaL. (p<0.05) treatment. The reduction of fibrosis positively correlated with TNF-αlevel (p<0.05,r=0.873). Methanolic extract of ceplukan leaf decreases ventricular fibrosis through the inhibition of ventricular TNF-αlevel in ovariectomized rats.

scholarly journals An investigation of bioactive and free radical scavenging potential of moringa Oliefera leaf extracts

2019 ◽  
Vol 10 (3) ◽  
pp. 1575-1579
Author(s):  
Uzma Sayyed ◽  
Pratibha Pandey ◽  
Rohit K. Tiwari ◽  
Rafia Shekh ◽  
Preeti Bajpai
Keyword(s):  
Methanolic Extract ◽  
Inflammatory Diseases ◽  
Radical Scavenging ◽  
Morphological Characteristics ◽  
Dependent Manner ◽  
Leaf Extracts ◽  
Ic50 Value ◽  
Percentage Yield ◽  
Antioxidant Potency ◽  
Dose Dependent

Moringa oleifera Lam, commonly known as Sehjan belongs to the Moringaceae family. It is widely used for the treatment of infectious and inflammatory diseases. This study was an attempt to evaluate the morphological characteristics, percent yield, the bioactive and antioxidant potential of M. oleifera leaves that would help in elucidating a promising therapeutic and curative agent for the treatment of different ailments. The maximum percentage yield was obtained in methanolic extract (29.55%) of M. oliefera leaves. Qualitative analysis also revealed the maximum presence of all the metabolites in methanolic extract. Quantitative analysis revealed an appreciable presence of phenol (53.1 mg/g) flavonoids (47.7mg/g) and carotenoids (16.46 mg/g) in M. oleifera leaves. The methanolic extract had shown the maximum antioxidant potency in a dose-dependent manner during the evaluation of enzymatic (SOD and CAT) and nonenzymatic (DPPH and FRAP) antioxidants with minimum IC50 value. Thus, it could be concluded from the present study that methanolic leaf extract of M. oliefera could be amongst the principle extract for the antioxidant activity of M. oliefera, which could be used for the treatment of several ailments.

scholarly journals Differential regulation of human dopamine D2 and somatostatin receptor subtype expression by glucocorticoids in vitro

2008 ◽  
Vol 42 (1) ◽  
pp. 47-56 ◽  
Author(s):  
C de Bruin ◽  
R A Feelders ◽  
A M Waaijers ◽  
P M van Koetsveld ◽  
D M Sprij-Mooij ◽  
...  
Keyword(s):  
Somatostatin Receptor ◽  
Receptor Subtype ◽  
Receptor Subtypes ◽  
Dependent Manner ◽  
Tt Cells ◽  
A Minor ◽  
Dose Dependent ◽  
Corticotroph Adenomas ◽  
Analogue Octreotide

Dopamine agonists (DA) and somatostatin (SS) analogues have been proposed in the treatment of ACTH-producing neuro-endocrine tumours that cause Cushing's syndrome. Inversely, glucocorticoids (GCs) can differentially influence DA receptor D2 or SS receptor subtype (sst) expression in rodent models. If this also occurs in human neuro-endocrine cells, then cortisol-lowering therapy could directly affect the expression of these target receptors. In this study, we investigated the effects of the GC dexamethasone (DEX) on D2 and sst expression in three human neuro-endocrine cell lines: BON (carcinoid) and TT (medullary thyroid carcinoma) versus DMS (small cell lung cancer), which is severely GC resistant. In BON and TT, sst2 mRNA was strongly down-regulated in a dose-dependent manner (IC50 0.84 nM and 0.16 nM), whereas sst5 and especially D2 were much more resistant to DEX treatment. Sst2 down-regulation was abrogated by a GC receptor antagonist and reversible in time upon GC withdrawal. At the protein level, DEX also induced a decrease in the total number of SS (−52%) and sst2-specific (−42%) binding sites. Pretreatment with DEX abrogated calcitonin inhibition by sst2-preferring analogue octreotide in TT. In DMS, DEX did not cause significant changes in the expression of these receptor subtypes. In conclusion, we show that GCs selectively down-regulate sst2, but not D2 and only to a minor degree sst5 in human neuro-endocrine BON and TT cells. This mechanism may also be responsible for the low expression of sst2 in corticotroph adenomas and underwrite the current interest in sst5 and D2 as possible therapeutic targets for a medical treatment of Cushing's disease.

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